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O/w type emulsion

An emulsion, independent technology, applied in the direction of emulsion delivery, allergic diseases, metabolic diseases, etc., to achieve the effect of high accumulation and high blood retention

Active Publication Date: 2018-07-31
NOF CORP +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is room for improvement in the intracellular drug release efficiency of these micelles and liposomes

Method used

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Examples

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preparation example Construction

[0272] The poorly water-soluble drug can be internally encapsulated in the O / W type emulsion of the present invention by performing emulsification using a lipid solution containing the poorly water-soluble drug dissolved therein in the preparation of the above O / W type emulsion. The present invention also provides the aforementioned O / W emulsion of the present invention in which a poorly water-soluble drug is encapsulated.

[0273] In the present invention, a poorly water-soluble drug refers to a drug having a water / octanol partition coefficient LogPow of not less than 4 for evaluating the hydrophobicity of a compound. Examples of such poorly water-soluble drugs include tacrolimus (LogPow: 4.79), ursodeoxycholic acid (LogPow: 4.76), oxicaine (LogPow: 4.38), simvastatin (LogPow: 4.72), ethinylestradiol Alcohol (LogPow: 4.11), Clotrimazole (LogPow: 4.93), Zaltoprofen (LogPow: 4.25), Betamethasone Valerate (LogPow: 4.14), Pentazocin (LogPow: 4.15), Iohexacic Acid (LogPow: 4.32),...

Embodiment 1

[0306] [Example 1] Preparation of fine O / W type emulsion

[0307] As cationic lipid, use B-2, B-2-5, O-C3M, B-2-3, TS-P4C2 or L-PZ4C2, prepare cationic lipid:DOPE:cholesterol=3:4: O / W type emulsion with a composition of 3 (molar ratio). In this preparation, as a model drug, 4-methylumbelliferone (10 mol%) was used, and as PEG lipids, DMG-PEG2000 (10 mol%) and DSG-PEG2000 (2.5 mol%) were used, and prepared 1.0 mM (based on lipid concentration) emulsion.

[0308] An ethanol solution containing 1000 nmol of the total amount of cationic lipid, DOPE, and cholesterol was prepared, and a model drug and PEG lipid were added in the above amounts. Ethanol was added so that the total amount was 400 μL, and the mixture was left standing at ice temperature for 15 minutes. Similarly ice-cold malic acid buffer (20 mM, pH 3.0, 30 mM NaCl) (400 μL) was mixed within 3 seconds under vortexing. PBS (NISSUI) (3200 μL) was immediately added thereto. The mixture was subjected to ultrafiltration...

Embodiment 2

[0319] [Example 2] Effect of pH on O / W Type Emulsion

[0320] As cationic lipid, use B-2 to prepare cationic lipid:DOPE:cholesterol=3:4:3 (molar ratio) or cationic lipid:DOPC:cholesterol=3:4:3 (molar ratio) The composition of the O / W type emulsion. In this preparation, as PEG lipid, DMG-PEG2000 (15 mol%) was used, and an emulsion of 0.5 mM (based on lipid concentration) was prepared.

[0321] An ethanol solution containing 500 nmol of the total amount of B-2, DOPE, and cholesterol was prepared, and PEG lipid was added in the above amount. Ethanol was added so that the total amount was 200 μL, and the mixture was left standing at ice temperature for 15 minutes. Similarly ice-cold malic acid buffer (20 mM, pH 3.0-pH 5.0) (200 μL) was mixed within 3 seconds under vortexing. PBS (NISSUI) (3600 μL) was immediately added thereto. The mixture was subjected to ultrafiltration using an Amicon Ultra (Millipore). Centrifugation conditions were 1000G, 25°C. The operation including a...

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Abstract

The present invention provides an O / W type emulsion which has a volume median diameter of 100 nm or less and which contains a compound represented by formula (1) (in the formula, Xa and Xb are each independently X1, X2 or a 1,4-piperazinediyl group, s is 1 or 2, R4 denotes an alkyl group having 1-6 carbon atoms, na and nb are each independently 0 or 1, R1a, R1b, R2a and R2b each independently denote an alkylene group having 1-6 carbon atoms, Ya and Yb each independently denote an ester bond or the like, and R3a and R3b each independently denote a fat-soluble vitamin residue or the like).

Description

technical field [0001] The present invention relates to an O / W type emulsion that disintegrates in response to a reducing environment in cells, and a method for preparing the same. Furthermore, the present invention relates to the use of the O / W type emulsion as a carrier for delivering poorly water-soluble drugs into cells. Background technique [0002] Most new drug candidates such as anticancer drugs, immunosuppressants, antibiotics, antifungal agents, antihyperlipidemic agents, antiinflammatory agents, etc. are poorly soluble in water. Even when they have sufficient pharmacological activity, development is often delayed or discontinued due to their difficulty in formulation. [0003] Conventionally, when a poorly water-soluble drug is applied to a pharmaceutical product, for example, solubilization with a hydrophilic surfactant or an inclusion compound such as cyclodextrin, or emulsification with vegetable oil and lecithin has been attempted . In order to achieve the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/20A61P37/06A61P35/00A61K31/37A61K31/573A61K45/00A61K47/22A61K47/24A61K47/28A61K47/10A61K9/107A61P29/00A61P3/06A61P31/00A61P31/04A61P31/10
CPCA61K47/20A61K47/22A61K31/37A61K31/573A61K9/1075A61K31/575A61P29/00A61P31/00A61P31/04A61P31/10A61P35/00A61P3/06A61P37/06A61K47/24A61K47/28A61K9/107
Inventor 丹下耕太中井悠太秋田英万田中浩挥渡边绫香三浦尚也原岛秀吉
Owner NOF CORP
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